EP0639372B1 - Device for distributing a therapeutic or cosmetic substance, where the inert carrier is hexamethyldisiloxane, and composition for use in this device - Google Patents

Device for distributing a therapeutic or cosmetic substance, where the inert carrier is hexamethyldisiloxane, and composition for use in this device Download PDF

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Publication number
EP0639372B1
EP0639372B1 EP94401864A EP94401864A EP0639372B1 EP 0639372 B1 EP0639372 B1 EP 0639372B1 EP 94401864 A EP94401864 A EP 94401864A EP 94401864 A EP94401864 A EP 94401864A EP 0639372 B1 EP0639372 B1 EP 0639372B1
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EP
European Patent Office
Prior art keywords
hexamethyldisiloxane
cosmetic
composition
active substance
therapeutic
Prior art date
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Expired - Lifetime
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EP94401864A
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German (de)
French (fr)
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EP0639372A1 (en
Inventor
James Appino
Jean-Marc Aiache
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Dow Corning France SAS
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Dow Corning France SAS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/046—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • A61K8/585—Organosilicon compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • C—CHEMISTRY; METALLURGY
    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K3/00—Materials not provided for elsewhere
    • C09K3/30—Materials not provided for elsewhere for aerosols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/87—Application Devices; Containers; Packaging
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00—Anti-perspirants or body deodorants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005—Antimicrobial preparations

Definitions

  • the present invention relates to a device for distribute a therapeutic substance in the form of aerosol particles or cosmetic;
  • It also relates to a sprayable composition intended in particular to be used in the device according to the invention and a method cosmetic treatment.
  • Aerosol cans for distributing various substances, especially for cosmetic or therapeutic use, and which include gases fluorocarbons (CFC or HFA) as propellants, are gradually prohibited given the harmful effects of said gases on the atmosphere.
  • gases fluorocarbons CFC or HFA
  • Some of these devices are formed of a rigid outer container and an elastic inner container the upper edge of which is attached to the outer container.
  • the outer container is surmounted by a valve holder cover placed on the upper edge of the outer container and a flow valve that extends into the container inside, a propellant being placed in the free space separating the outer container inner container.
  • the propellant discharges the product contained in the inner container to the outside by the valve flow which is then opened.
  • Other devices consist of a rigid container surmounted a pump body comprising a variable volume pump chamber, the interior of which is housed a piston, with an entry hole to establish a chamber filling communication with the container and a hole outlet to allow emission to the outside of the active substance.
  • the propellant is supplied by the compression of a fluid, which is the more often air inside the container by means of actuation piston of the pump chamber.
  • US Patent 4,346,079 proposes an antiperspirant composition containing a gelled alcoholic solution of an antiperspirant compound, the gelling agent comprising fatty acid salts such as stearate sodium and a small amount of a siloxane whose viscosity is understood between 0.01 and 25 centistokes such as polydimethylsiloxanes, polyphenylmethylsiloxanes and cyclic polydimethylsiloxanes.
  • patent application EP-A-0 211 555 describes a transparent silicone composition comprising a small amount of an alcohol liquid fat or liquid polyoxyalkyl alcohol.
  • the document quotes linear or cyclic polymethylsiloxanes having one to six methylsiloxanes.
  • These compositions find an application in cosmetics (shampoos, deodorants, antiperspirants, lotions and
  • the volatile silicones in these realizations are vehicles ensuring good spreading of the active substance and / or a good penetration thereof when the composition has already been deposited on the medium to be treated.
  • Document DE 38 10730 describes a sprayable composition cosmetic which includes an amount of hexamethyldisiloxane which cannot give satisfactory results within the framework of a distribution system in the form of aerosol particles of a therapeutic substance or cosmetic.
  • EP-A-468 564 describes a cosmetic composition in which in Example 1 the volatile silicone is Dow Corning 345 (pentamer).
  • Document DE 33 30 447 indicates very generally the use of dimethylsiloxane polymer for aerosols (page 7, lines 13 to 16).
  • Document EP 478 456 describes an antifungal composition under dry spray form incorporating various silicones.
  • hexamethyldisiloxane of sufficient volatility could be used as an inert carrier of aerosol dispensing devices of an active substance therapeutic or cosmetic.
  • the object of the present invention is therefore to propose a device comprising such an inert vehicle and allowing an all-purpose application completely satisfactory of the active substance on the skin.
  • the term inert vehicle is used to designate the dispersion medium which will bring the active substance of the interior of the reservoir to the support to be treated.
  • the devices which are used in the context of the present invention may comprise on the one hand a propellant gas and on the other hand a vehicle inert. These devices can be of the twin-pocket or chamber type variable volume pump.
  • the two-pocket devices are formed of a container internal elastic containing the composition and a rigid external container, the free space separating the external container from the internal container being occupied by a propellant.
  • Volume pump chamber devices variable are formed by a rigid container containing the composition, associated to a pump chamber communicating with said container.
  • They can also be of the type including the pump piston which is in the chamber, actuated by the pusher, allows the expulsion of the composition without requiring the action of propellants.
  • These devices are particularly preferred and an example of such a device is that marketed by the company Valois Pharm. (France), under the reference VP3.
  • Hexamethyldisiloxane is produced for example by the company DOW-CORNING and carries the reference Q7-9179 or by RHONE POULENC reference Silbione Oil 70041 V 0.65, The physicochemical properties of this product are particularly described in the commercial brochures edited by these companies. These compounds are also known for their compatibility with use in cosmetics or dermatology under topical form.
  • these compounds have a higher purity or preferably equal to 99% or advantageously 99.2% and pass through a 400 mesh sieve.
  • the inert vehicle and the active substance form a mixture thixotropic, i.e. it is at rest in the form of gel while the application of a movement from top to bottom, in particular, allows the transform back into liquid ready to be expelled under the action of the propellant.
  • composition comprising the inert vehicle a known agent to improve thixotropy.
  • This agent will in particular be based on silica as the compound known under the brand name Aérosil® (marketed by the company DEGUSSA).
  • composition will advantageously include densification charges, in particular based on silica such as talc and additives improving the presentation of the mixture, in particular olfactory perfumes.
  • composition will either be in the form of a solution when the substance active is soluble in the inert vehicle, either as a suspension in insolubility of the active substance in the inert vehicle.
  • the active substance transported in dispersed form by the vehicle can be either in liquid form or in solid form.
  • the active substance will be transported in the form of powder and therefore the compounds forming the active substance will be chosen among those which form a suspension in the vehicle inert.
  • an antifungal such as imidazoles or triazoles, especially econazole base.
  • antifungals can also be used in the context of the present invention.
  • the single attached figure illustrates a dual-pocket device as it is known in the art, which may be suitable to the implementation of the present invention.
  • the figure shows a half section along the longitudinal axis of a such device.
  • the dispensing device 1 comprises a rigid external container body 2 consisting of a bottom 3 from which extends vertically upwards a finished peripheral side wall 4 at its upper end by a converging wall 5.
  • a container interior of flexible elastic material 6 containing composition 7 of active substance and inert vehicle is housed inside the body of container, the edge of the inner container being attached to the outer container and a valve holder cover 8 being placed on the upper edge of the container exterior and being surmounted by a flow valve 9 which extends into the outer container with a bent tip 10.
  • a propellant 11 is placed in the free space separating the body from outer container to inner container.
  • the angled end piece 10 at its upper end is connected to the nozzle 12 and then at the opening 14 of the distribution device by actuation of the push button 13.
  • the invention can also be implemented using devices comprising a variable volume pump chamber as described by example in patent applications FR-A-2 436 (0) 85 and 2 663 909 or as they are well known to those skilled in the art.
  • the invention also relates to the use of hexamethyldisiloxane as an inert vehicle in the distribution of aerosol particles according to the invention.
  • the invention also relates to a treatment method cosmetic of the skin, characterized in that it is applied to a place of this an effective dose of an active substance using a device such as previously described.
  • the applied substance is for cosmetic use and is in particular in the form of a powder.
  • the layer thus deposited has a uniformity and remarkable homogeneity that it's not possible reach with other inert vehicles.
  • inert vehicles based on compounds are used fluorocarbons such as HFA or CFC
  • the pulverized material present in the form of a mist whose application cannot be directed as effectively as when using the inert vehicle according to the invention.
  • the propellant occupying the free space between the two receptacles is nitrogen.
  • the pressure exerted on the pocket (flexible tank) is 8 bars.
  • Pressurization can also be carried out by a pump mechanical.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Birds (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
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  • Compositions Of Macromolecular Compounds (AREA)

Abstract

The present invention relates to a device which makes it possible to distribute, in the form of aerosol particles, a therapeutic or cosmetic substance. The device according to the invention is of the double pouch type or of a type surmounted by a pump assembly and is characterised in that it contains a composition comprising an active substance and an inert vehicle which is one or more polydiorganosiloxanes of sufficient volatility to ensure the expulsion of the composition in the form of aerosol particles. The invention also relates to the composition intended to be used in the device.

Description

La présente invention concerne un dispositif permettant de distribuer sous forme de particules d'aérosol une substance thérapeutique ou cosmétique;The present invention relates to a device for distribute a therapeutic substance in the form of aerosol particles or cosmetic;

Elle concerne également une composition pulvérisable destinée notamment à être utilisée dans le dispositif selon l'Invention et un procédé de traitement cosmétique.It also relates to a sprayable composition intended in particular to be used in the device according to the invention and a method cosmetic treatment.

Les bombes aérosols permettant de distribuer diverses substances, notamment à usage cosmétique ou thérapeutique, et qui comprennent des gaz fluorocarbonés (CFC ou HFA) comme gaz propulseurs, sont progressivement interdites compte tenu des effets néfastes desdits gaz sur l'atmosphère.Aerosol cans for distributing various substances, especially for cosmetic or therapeutic use, and which include gases fluorocarbons (CFC or HFA) as propellants, are gradually prohibited given the harmful effects of said gases on the atmosphere.

Afin de remplacer les gaz propulseurs fluorocarbonés, on a proposé différents dispositifs faisant intervenir d'une part un gaz propulseur (non fluorocarboné) et d'autre part, un véhicule inerte permettant d'accompagner la substance active jusqu'à son lieu d'application.In order to replace fluorocarbon propellants, we have proposed different devices involving on the one hand a propellant (not fluorocarbon) and on the other hand, an inert vehicle allowing to accompany the active substance to its place of application.

Certains de ces dispositifs appelés communément bi-poches sont formés d'un récipient extérieur rigide et d'un récipient intérieur élastique dont le bord supérieur est fixé au récipient extérieur. Le récipient extérieur est surmonté d'un couvercle porte-valve posé sur le bord supérieur du récipient extérieur et d'une valve de débit qui s'étend dans le récipient intérieur, un gaz propulseur étant placé dans l'espace libre séparant le récipient extérieur du récipient intérieur.Some of these devices, commonly known as two-pocket devices, are formed of a rigid outer container and an elastic inner container the upper edge of which is attached to the outer container. The outer container is surmounted by a valve holder cover placed on the upper edge of the outer container and a flow valve that extends into the container inside, a propellant being placed in the free space separating the outer container inner container.

Lorsque la valve de débit est actionnée, le gaz propulseur refoule le produit contenu dans le récipient intérieur vers l'extérieur par la valve de débit qui est alors ouverte.When the flow valve is actuated, the propellant discharges the product contained in the inner container to the outside by the valve flow which is then opened.

Ces dispositifs sont notamment décrits dans les demandes de brevet FR-A-2 436 085 ou FR-A-2 663 909.These devices are notably described in patent applications FR-A-2 436 085 or FR-A-2 663 909.

D'autres dispositifs sont constitués d'un récipient rigide surmonté d'un corps de pompe comprenant une chambre de pompe à volume variable, à l'intérieur de laquelle est logé un piston, avec un trou d'entrée pour établir une communication de remplissage de la chambre avec le récipient et un trou de sortie pour permettre l'émission à l'extérieur de la substance active. Dans ce cas, le gaz propulseur est fourni par la compression d'un fluide, qui est le plus souvent de l'air, à l'intérieur du récipient au moyen de l'actionnement du piston de la chambre de pompe. Other devices consist of a rigid container surmounted a pump body comprising a variable volume pump chamber, the interior of which is housed a piston, with an entry hole to establish a chamber filling communication with the container and a hole outlet to allow emission to the outside of the active substance. In in this case, the propellant is supplied by the compression of a fluid, which is the more often air inside the container by means of actuation piston of the pump chamber.

Ces dispositifs sont notamment décrits dans les demandes de brevet FR-A-2 647 418 et FR-A-2 643 338.These devices are notably described in patent applications FR-A-2 647 418 and FR-A-2 643 338.

Néanmoins les véhicules inertes contenus dans les récipients en mélange avec la substance active présentent certains inconvénients liés à leur nature chimique propre ce qui rend le fonctionnement de tels dispositifs peu satisfaisants.However, the inert vehicles contained in the containers in mixture with the active substance have certain drawbacks related to their own chemical nature which makes the functioning of such devices unsatisfactory.

C'est le cas notamment des véhicules inertes à base d'alcool éthylique.This is particularly the case for inert alcohol-based vehicles ethyl.

On connaít par ailleurs l'utilisation en cosmétique ou en médecine pour des applications topiques de solutions, gels ou bâtonnets comportant comme substance favorisant l'étalement, des polydiorganosiloxanes.We also know the use in cosmetics or medicine for topical applications of solutions, gels or sticks comprising as the spreading substance, polydiorganosiloxanes.

Le brevet US 4 346 079 propose une composition anti-transpirante contenant une solution alcoolique gélifiée d'un composé anti-transpirant, l'agent gélifiant comprenants des sels d'acide gras tels que le stéarate de sodium et une faible quantité d'un siloxane dont la viscosité est comprise entre 0,01 à 25 centistokes comme les polydiméthylsiloxanes, les polyphénylméthylsiloxanes et les polydiméthylsiloxanes cycliques.US Patent 4,346,079 proposes an antiperspirant composition containing a gelled alcoholic solution of an antiperspirant compound, the gelling agent comprising fatty acid salts such as stearate sodium and a small amount of a siloxane whose viscosity is understood between 0.01 and 25 centistokes such as polydimethylsiloxanes, polyphenylmethylsiloxanes and cyclic polydimethylsiloxanes.

Par ailleurs, la demande de brevet EP-A-0 211 555 décrit une composition silicone transparente comportant une faible quantité d'un alcool gras liquide ou d'un alcool polyoxyalcoylé liquide. Parmi les silicones utilisés, le document cite les polyméthylsiloxanes linéaires ou cycliques ayant un à six méthylsiloxanes. Ces compositions trouvent une application en cosmétique (shampooings, déodorants, anti-transpirants, lotions et parfums) En d'autres termes, les silicones volatils dans ces réalisations sont des véhicules assurant un bon étalement de la substance active et/ou une bonne pénétration de celle-ci lorsque la composition a déjà été déposée sur le support à traiter.Furthermore, patent application EP-A-0 211 555 describes a transparent silicone composition comprising a small amount of an alcohol liquid fat or liquid polyoxyalkyl alcohol. Among the silicones used, the document quotes linear or cyclic polymethylsiloxanes having one to six methylsiloxanes. These compositions find an application in cosmetics (shampoos, deodorants, antiperspirants, lotions and In other words, the volatile silicones in these realizations are vehicles ensuring good spreading of the active substance and / or a good penetration thereof when the composition has already been deposited on the medium to be treated.

Le document DE 38 10730 décrit une composition pulvérisable cosmétique qui comprend une quantité d'hexaméthyldisiloxane qui ne peut donner de résultats satisfaisants dans le cadre d'un dispositif de distribution sous forme de particules d'aérosol d'une substance thérapeutique ou cosmétique. Document DE 38 10730 describes a sprayable composition cosmetic which includes an amount of hexamethyldisiloxane which cannot give satisfactory results within the framework of a distribution system in the form of aerosol particles of a therapeutic substance or cosmetic.

Le document EP-A-468 564 décrit une composition cosmétique dans laquelle à l'exemple 1 le silicone volatil est le Dow Corning 345 (pentamer).EP-A-468 564 describes a cosmetic composition in which in Example 1 the volatile silicone is Dow Corning 345 (pentamer).

Le document DE 33 30 447 indique de manière très générale l'utilisation de polymère de diméthylsiloxane pour les aérosols (page 7, lignes 13 à 16).Document DE 33 30 447 indicates very generally the use of dimethylsiloxane polymer for aerosols (page 7, lines 13 to 16).

Le document EP 478 456 décrit une composition antifongique sous forme de spray sec incorporant divers silicones.Document EP 478 456 describes an antifungal composition under dry spray form incorporating various silicones.

De façon inattendue, on a trouvé que l'hexaméthyldisiloxane de volatilité suffisante pouvaient être utilisés en tant que véhicule inerte des dispositifs de distribution sous forme d'aérosol d'une substance active thérapeutique ou cosmétique.Unexpectedly, it was found that the hexamethyldisiloxane of sufficient volatility could be used as an inert carrier of aerosol dispensing devices of an active substance therapeutic or cosmetic.

L'objet de la présente invention est donc de proposer un dispositif comportant un tel véhicule inerte et permettant une application tout à fait satisfaisante de la substance active sur la peau.The object of the present invention is therefore to propose a device comprising such an inert vehicle and allowing an all-purpose application completely satisfactory of the active substance on the skin.

Selon l'invention, le terme de véhicule inerte est employé pour désigner le milieu de dispersion qui amènera la substance active de l'intérieur du réservoir au support à traiter.According to the invention, the term inert vehicle is used to designate the dispersion medium which will bring the active substance of the interior of the reservoir to the support to be treated.

Il s'agit donc d'une fonction disjointe de celle consistant à faciliter l'étalement sur la peau d'une composition qui y a déjà été déposée par un moyen approprié.It is therefore a function separate from that of facilitating spreading on the skin of a composition which has already been deposited therein by a appropriate means.

Par ailleurs, on a constaté de façon inattendue que le dépôt ainsi obtenu par l'utilisation du dispositif présentait une grande homogénéité et une grande régularité, tout en procurant une sensation agréable comparée aux dépôts similaires effectués par d'autres moyens.Furthermore, it was unexpectedly found that the deposit thus obtained by the use of the device exhibited great homogeneity and great regularity, while providing a pleasant feeling compared similar deposits made by other means.

L'invention est donc relative à un dispositif, permettant de distribuer sous forme d'aérosol une substance active thérapeutique ou cosmétique, constitué d'un récipient contenant une composition comportant la substance active et un véhicule inerte, d'une valve de débit s'étendant dans ledit récipient et d'un moyen de propulsion caractérisé en ce que la composition consiste, en pourcentage en poids, en:

  • 75 à 95 % d'hexaméthyldisiloxane.
  • 0,01 à 15 % de substance thérapeutique ou cosmétique,
  • 0 à 10 % d'agent améliorant la thixotropie, de préférence au moins 1%,
  • 0 à 20 % de charges de densitification ou additifs cosmétiques.
The invention therefore relates to a device, making it possible to distribute, in the form of an aerosol, a therapeutic or cosmetic active substance, consisting of a container containing a composition comprising the active substance and an inert vehicle, of a flow valve s' extending into said container and a propelling means characterized in that the composition consists, in percentage by weight, of:
  • 75 to 95% hexamethyldisiloxane.
  • 0.01 to 15% of therapeutic or cosmetic substance,
  • 0 to 10% of thixotropy improving agent, preferably at least 1%,
  • 0 to 20% densification charges or cosmetic additives.

Les dispositifs qui sont utilisés dans le cadre de la présente invention peuvent comporter d'une part un gaz propulseur et d'autre part un véhicule inerte. Ces dispositifs peuvent être du type bi-poche ou à chambre de pompe à volume variable.The devices which are used in the context of the present invention may comprise on the one hand a propellant gas and on the other hand a vehicle inert. These devices can be of the twin-pocket or chamber type variable volume pump.

De façon connue, les dispositifs bi-poches sont formés d'un récipient interne élastique contenant la composition et d'un récipient externe rigide, l'espace libre séparant le récipient externe du récipient interne étant occupé par un gaz propulseur. Les dispositifs à chambre de pompe à volume variable sont formés d'un récipient rigide contenant la composition, associé à une chambre de pompe communicant avec ledit récipient.In known manner, the two-pocket devices are formed of a container internal elastic containing the composition and a rigid external container, the free space separating the external container from the internal container being occupied by a propellant. Volume pump chamber devices variable are formed by a rigid container containing the composition, associated to a pump chamber communicating with said container.

Ils peuvent être également du type dont le piston de la pompe qui est dans la chambre, actionné par le poussoir, permet l'expulsion de la composition sans nécessiter l'action de gaz propulsifs. Ces dispositifs sont particulièrement préférés et un exemple d'un tel dispositif est celui commercialisé par la société Valois Pharm. (France), sous la référence VP3.They can also be of the type including the pump piston which is in the chamber, actuated by the pusher, allows the expulsion of the composition without requiring the action of propellants. These devices are particularly preferred and an example of such a device is that marketed by the company Valois Pharm. (France), under the reference VP3.

L'hexaméthyldisiloxane est fabriqué par exemple par la société DOW-CORNING et porte la référence Q7-9179 ou par RHONE POULENC référence Silbione Huile 70041 V 0,65, Les propriétés physico-chimiques de ce produit sont notamment décrites dans les brochures commerciales éditées par ces sociétés. Ces composés sont par ailleurs connus pour leur compatibilité avec une utilisation en cosmétique ou en dermatologie sous forme topique. Hexamethyldisiloxane is produced for example by the company DOW-CORNING and carries the reference Q7-9179 or by RHONE POULENC reference Silbione Oil 70041 V 0.65, The physicochemical properties of this product are particularly described in the commercial brochures edited by these companies. These compounds are also known for their compatibility with use in cosmetics or dermatology under topical form.

De préférence, ces composés présentent une pureté supérieure ou égale, de préférence supérieure, à 99 % ou avantageusement 99,2 % et passent au tamis de 400 mesh.Preferably, these compounds have a higher purity or preferably equal to 99% or advantageously 99.2% and pass through a 400 mesh sieve.

Le véhicule inerte et la substance active forment un mélange thixotrope, c'est-à-dire qu'il est au repos sous forme de gel alors que l'application d'un mouvement de haut en bas, notamment, permet de le retransformer en liquide prêt à être expulsé sous l'action du gaz propulseur.The inert vehicle and the active substance form a mixture thixotropic, i.e. it is at rest in the form of gel while the application of a movement from top to bottom, in particular, allows the transform back into liquid ready to be expelled under the action of the propellant.

Afin d'améliorer le caractère thixotrope du mélange, il est avantageux d'ajouter à la composition comportant le véhicule inerte un agent connu pour améliorer la thixotropie. Cet agent sera notamment à base de silice comme le composé connu sous le nom de marque Aérosil® (commercialisé par la société DEGUSSA).In order to improve the thixotropic nature of the mixture, it is advantageous adding to the composition comprising the inert vehicle a known agent to improve thixotropy. This agent will in particular be based on silica as the compound known under the brand name Aérosil® (marketed by the company DEGUSSA).

Par ailleurs la composition comprendra avantageusement des charges de densification, notamment à base de silice comme le talc et des additifs améliorant la présentation notamment olfactive du mélange comme des parfums.Furthermore, the composition will advantageously include densification charges, in particular based on silica such as talc and additives improving the presentation of the mixture, in particular olfactory perfumes.

La composition sera soit sous forme de solution lorsque la substance active est soluble dans le véhicule inerte, soit sous forme de suspension en cas d'insolubilité de la substance active dans le véhicule inerte.The composition will either be in the form of a solution when the substance active is soluble in the inert vehicle, either as a suspension in insolubility of the active substance in the inert vehicle.

Ainsi, la substance active transportée sous forme dispersée par le véhicule peut être soit sous forme liquide, soit sous forme solide.Thus, the active substance transported in dispersed form by the vehicle can be either in liquid form or in solid form.

De préférence, la substance active sera transportée sous forme de poudre et en conséquence, les composés formant la substance active seront choisis parmi ceux qui forment une suspension dans le véhicule inerte.Preferably, the active substance will be transported in the form of powder and therefore the compounds forming the active substance will be chosen among those which form a suspension in the vehicle inert.

Parmi ces composés, il est avantageux d'utiliser comme substance active un antifongique comme les imidazoles ou les triazoles, notamment à base d'éconazole. Bien entendu, d'autres antifongiques peuvent également être utilisés dans le cadre de la présente invention.Among these compounds, it is advantageous to use as substance activates an antifungal such as imidazoles or triazoles, especially econazole base. Of course, other antifungals can also be used in the context of the present invention.

Comme autres substances actives pouvant être utilisées avantageusement dans le cadre de l'invention, on peut citer notamment les produits cosmétiques suivants: "Déodorants, antiperspirants, antiseptiques cutanés et les produits pharmaceutiques choisis parmi les hémostatiques, les antibiotiques, les polymères protecteurs, cicatrisants, les hormones, les substances absorbées par la peau capables d'une activité générale (cardiotonique par ex.)".As other active substances which can be used advantageously in the context of the invention, there may be mentioned in particular the following cosmetic products: "Deodorants, antiperspirants, antiseptics skin and pharmaceutical products chosen from hemostats, antibiotics, protective, healing polymers, hormones, substances absorbed by the skin capable of general activity (eg cardiotonic) ".

De préférence, la composition pulvérisable consiste en pourcentage en poids en:

  • 80 à 90 % d'hexaméthyldisiloxane,
  • 0,1 à 5 % de substance thérapeutique ou cosmétique,
  • 0 à 10 % d'agent améliorant la thixotropie de préférence au moins 1%,
  • 0 à 20 % de charges ou additifs, de préférence au moins 5 %.
Preferably, the sprayable composition consists in percentage by weight of:
  • 80 to 90% hexamethyldisiloxane,
  • 0.1 to 5% of therapeutic or cosmetic substance,
  • 0 to 10% of thixotropy improving agent, preferably at least 1%,
  • 0 to 20% of fillers or additives, preferably at least 5%.

A titre d'illustration de la présente invention la figure unique ci-jointe illustre un dispositif bi-poche tel qu'il est connu dans l'art, pouvant convenir à la mise en oeuvre de la présente invention.By way of illustration of the present invention, the single attached figure illustrates a dual-pocket device as it is known in the art, which may be suitable to the implementation of the present invention.

La figure représente une demie coupe selon l'axe longitudinal d'un tels dispositif.The figure shows a half section along the longitudinal axis of a such device.

Conformément à cette figure, le dispositif distributeur 1 comporte un corps de récipient externe rigide 2 constitué d'un fond 3 à partir duquel s'étend verticalement vers le haut une paroi latérale périphérique 4 terminée à son extrémité supérieure par une paroi convergente 5. Un récipient intérieur en matière élastique souple 6 contenant la composition 7 de substance active et de véhicule inerte est logé à l'intérieur du corps de récipient, le bord du récipient intérieur étant fixé au récipient extérieur et un couvercle porte-valve 8 étant posé sur le bord supérieur du récipient extérieur et étant surmonté d'une valve de débit 9 qui s'étend dans le récipient extérieur par un embout coudé 10.According to this figure, the dispensing device 1 comprises a rigid external container body 2 consisting of a bottom 3 from which extends vertically upwards a finished peripheral side wall 4 at its upper end by a converging wall 5. A container interior of flexible elastic material 6 containing composition 7 of active substance and inert vehicle is housed inside the body of container, the edge of the inner container being attached to the outer container and a valve holder cover 8 being placed on the upper edge of the container exterior and being surmounted by a flow valve 9 which extends into the outer container with a bent tip 10.

Un gaz propulseur 11 est placé dans l'espace libre séparant le corps de récipient extérieur du récipient intérieur.A propellant 11 is placed in the free space separating the body from outer container to inner container.

L'embout coudé 10 à son extrémité supérieure est relié à la buse d'admission 12 puis à l'ouverture 14 du dispositif de distribution par l'actionnement du bouton poussoir 13.The angled end piece 10 at its upper end is connected to the nozzle 12 and then at the opening 14 of the distribution device by actuation of the push button 13.

L'invention peut également être réalisée à l'aide de dispositifs comprenant une chambre de pompe à volume variable comme décrit par exemple dans les demandes de brevet FR-A-2 436 (0)85 et 2 663 909 ou tels qu'ils sont bien connus de l'homme du métier.The invention can also be implemented using devices comprising a variable volume pump chamber as described by example in patent applications FR-A-2 436 (0) 85 and 2 663 909 or as they are well known to those skilled in the art.

L'invention a également pour objet une composition pulvérisable destinée notamment à être utilisée dans un dispositif tel qu'il vient d'être décrit précédemment et consistant en pourcentage en poids en :

  • 75 à 95 % de d'hexaméthyldisiloxane,
  • 0,01 à 15 % de substance thérapeutique ou cosmétique,
  • 0 à 10 % d'agent améliorant la thixotropie de préférence au moins 1 %,
  • 0 à 20 % de charges ou additifs.
The subject of the invention is also a sprayable composition intended in particular for use in a device as just described above and consisting of percentage by weight in:
  • 75 to 95% of hexamethyldisiloxane,
  • 0.01 to 15% of therapeutic or cosmetic substance,
  • 0 to 10% of thixotropy improving agent, preferably at least 1%,
  • 0 to 20% of fillers or additives.

L'invention a également pour objet l'utilisation de l'hexaméthyldisiloxane comme véhicule inerte dans les dispositifs de distribution de particules d'aérosol selon l'invention.The invention also relates to the use of hexamethyldisiloxane as an inert vehicle in the distribution of aerosol particles according to the invention.

L'invention a également pour objet un procédé de traitement cosmétique de la peau, caractérisé en ce qu'on applique à un endroit de celle-ci une dose efficace d'une substance active à l'aide d'un dispositif tel que décrit précédemment.The invention also relates to a treatment method cosmetic of the skin, characterized in that it is applied to a place of this an effective dose of an active substance using a device such as previously described.

Selon une variante, la substance appliquée est à usage cosmétique et est notamment sous la forme d'une poudre.According to a variant, the applied substance is for cosmetic use and is in particular in the form of a powder.

De façon inattendue, la couche ainsi déposée présente une uniformité et une homogénéité remarquable qu'il n'est pas possible d'atteindre avec les autres véhicules inertes.Unexpectedly, the layer thus deposited has a uniformity and remarkable homogeneity that it's not possible reach with other inert vehicles.

Par ailleurs, si l'on utilise des véhicules inertes à base de composés fluorocarbonés tels que les HFA ou les CFC, la matière pulvérisée se présente sous la forme d'un brouillard dont l'application ne peut être dirigée de façon aussi efficace que lorsque l'on utilise le véhicule inerte selon l'invention.In addition, if inert vehicles based on compounds are used fluorocarbons such as HFA or CFC, the pulverized material present in the form of a mist whose application cannot be directed as effectively as when using the inert vehicle according to the invention.

L'invention est maintenant illustrée par un exemple de réalisation donné à titre illustratif.The invention is now illustrated by an exemplary embodiment given by way of illustration.

La composition suivante est utilisée :

  • nitrate d'éconazole 0,2 g,
  • talc 2 g
  • Aérosil 200 (silice colloïdale ) 0,6 g
  • hexaméthyldisiloxane 17,16 g commercialisé par la société Dow Corning sous la référence Q7-9179,
  • parfum 0,04 g
The following composition is used:
  • 0.2 g econazole nitrate,
  • talc 2 g
  • Aerosil 200 (colloidal silica) 0.6 g
  • hexamethyldisiloxane 17.16 g sold by the company Dow Corning under the reference Q7-9179,
  • perfume 0.04 g

Le propulseur occupant l'espace libre entre les deux récipients est de l'azote. La pression exercée sur la poche (réservoir souple) est de 8 bars.The propellant occupying the free space between the two receptacles is nitrogen. The pressure exerted on the pocket (flexible tank) is 8 bars.

La mise sous pression peut également être exercée par une pompe mécanique.Pressurization can also be carried out by a pump mechanical.

Claims (15)

  1. Device enabling a therapeutic or cosmetic active substance to be dispensed in the form of aerosol particles, consisting of a container (6) containing a composition (7) including the active substance and an inert vehicle, a flow valve (9) extending into the said container and a means of propulsion (11), characterized in that the composition consists, in percentage by weight, of:
    75 to 95% of hexamethyldisiloxane,
    0.01 to 15% of therapeutic or cosmetic substance,
    0 to 10% of agent improving the thixotropy, preferably at least 1%, and
    0 to 20% of cosmetic additives or densifying fillers.
  2. Device according to Claim 1, characterized in that the composition comprises an agent based on silica which improves the thixotropy of the said vehicle.
  3. Device according to Claim 1, characterized in that the active substance is in powder form.
  4. Device according to one of Claims 1 to 3, characterized in that the active substance is an antifungal agent, in particular one which is based on econazole.
  5. Device according to one of the preceding claims, characterized in that it is of the two-compartment type.
  6. Device according to one of Claims 1 to 4, characterized in that it is of the variable-volume pump chamber type.
  7. Cosmetic or pharmaceutical sprayable composition consisting in percentage by weight of:
    75 to 95% of hexamethyldisiloxane,
    0.01 to 15% of therapeutic or cosmetic substance,
    0 to 10% of agent improving the thixotropy, preferably at least 1%, and
    0 to 20% of fillers or additives, preferably at least 5%.
  8. Sprayable composition according to Claim 7, consisting in percentage by weight of:
    80 to 90% of hexamethyldisiloxane,
    0.1 to 5% of therapeutic or cosmetic substance,
    0 to 10% of agent improving the thixotropy, preferably at least 1%, and
    0 to 20% of fillers or additives, preferably at least 5%.
  9. Cosmetic treatment process for the skin, characterized in that an effective dose of an active substance is applied to an area of the skin using a device according to one of Claims 1 to 6.
  10. Use of hexamethyldisiloxane as an inert vehicle in the manufacture of a cosmetic or pharmaceutical product intended to be presented in the form of an aerosol particle distributor, characterized in that the product composition consists, in percentage by weight, of:
    75 to 95% of hexamethyldisiloxane,
    0.01 to 15% of therapeutic or cosmetic substance,
    0 to 10% of agent improving the thixotropy, preferably at least 1%,
    0 to 20% of cosmetic additives or densifying fillers.
  11. Use of hexamethyldisiloxane according to Claim 10, characterized in that the composition comprises an agent based on silica which improves the thixotropy of the vehicle.
  12. Use of hexamethyldisiloxane according to either of Claims 10 and 11, characterized in that the active substance is in powder form.
  13. Use of hexamethyldisiloxane according to one of Claims 10 to 12, characterized in that the active substance is an antifungal agent, in particular one which is based on econazole.
  14. Use of hexamethyldisiloxane according to one of Claims 10 to 13, characterized in that the aerosol particle distributor is of two-compartment type.
  15. Use of hexamethyldisiloxane according to one of Claims 10 to 13, characterized in that the aerosol particle distributor is of the variable-volume pump chamber type.
EP94401864A 1993-08-18 1994-08-17 Device for distributing a therapeutic or cosmetic substance, where the inert carrier is hexamethyldisiloxane, and composition for use in this device Expired - Lifetime EP0639372B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9310075A FR2709131B1 (en) 1993-08-18 1993-08-18 Device for dispensing a therapeutic or cosmetic substance, the inert vehicle of which is a volatile polydiorganosiloxane, and composition intended for use in the device.
FR9310075 1993-08-18

Publications (2)

Publication Number Publication Date
EP0639372A1 EP0639372A1 (en) 1995-02-22
EP0639372B1 true EP0639372B1 (en) 2002-11-13

Family

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EP94401864A Expired - Lifetime EP0639372B1 (en) 1993-08-18 1994-08-17 Device for distributing a therapeutic or cosmetic substance, where the inert carrier is hexamethyldisiloxane, and composition for use in this device

Country Status (7)

Country Link
US (1) US5582815A (en)
EP (1) EP0639372B1 (en)
JP (1) JPH07233091A (en)
AT (1) ATE227562T1 (en)
CA (1) CA2130305C (en)
DE (1) DE69431700T2 (en)
FR (1) FR2709131B1 (en)

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Publication number Priority date Publication date Assignee Title
US6861046B1 (en) * 1993-08-18 2005-03-01 Dow Corning France Device for dispensing a therapeutic or cosmetic substance onto the skin and a method of skin treatment
WO1998041154A1 (en) 1997-03-20 1998-09-24 Focal, Inc. Biodegradable tissue retractor
US6258857B1 (en) * 1999-02-04 2001-07-10 Kyowa Industrial Co., Ltd. Internal liquid composition contained as internal liquid in a releasing container and releasing container product
DE10024413A1 (en) * 2000-05-19 2001-12-06 Mika Pharma Gmbh Pharmaceutical and / or cosmetic preparation
EP1539098B1 (en) * 2002-09-20 2011-08-10 Fmc Corporation Cosmetic composition containing microcrystalline cellulose
WO2005123090A1 (en) 2004-06-17 2005-12-29 Galderma S.A. Composition in spray form comprising a combination of a corticoid and a vitamin d derivative in an oily phase
FR2871697B1 (en) * 2004-06-17 2007-06-29 Galderma Sa SPRAY COMPOSITION COMPRISING AN ASSOCIATION OF PHARMACEUTICAL ASSETS, AN ALCOHOLIC PHASE, AT LEAST ONE VOLATILE SILICONE AND A NON-VOLATILE OIL PHASE
FR2871698B1 (en) * 2004-06-17 2008-07-04 Galderma Sa SPRAY COMPOSITION COMPRISING AN ASSOCIATION OF PHARMACEUTICAL ASSETS AND AN OILY PHASE
EP1928415A2 (en) * 2005-08-13 2008-06-11 Collegium Pharmaceutical, Inc. Topical delivery with a carrier fluid
HUP0900072A2 (en) * 2009-02-06 2010-09-28 Egis Gyogyszergyar Nyilvanosan Transdermal pharmaceutical compositions
HU227970B1 (en) * 2007-07-10 2012-07-30 Egis Gyogyszergyar Nyrt Pharmaceutical compositions containing silicones of high volatility
AP3434A (en) * 2010-07-19 2015-10-31 Egis Semisolid pharmaceutical formulations
US11154535B2 (en) 2012-07-31 2021-10-26 Egis Pharmaceuticals Plc Transdermal formulation containing COX inhibitors
US10045935B2 (en) 2012-07-31 2018-08-14 Egis Pharmaceuticals Plc Transdermal formulation containing COX inhibitors
US20170121098A1 (en) * 2015-11-02 2017-05-04 American Sterilizer Company Non-aspirating transport gel dispenser

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JPS62164615A (en) * 1986-01-14 1987-07-21 Kao Corp Anhidrotic composition for spray
DE3810730A1 (en) * 1988-03-30 1989-10-12 Desitin Arzneimittel Gmbh Sprayable ointment composition
US5292530A (en) * 1991-06-02 1994-03-08 Helene Curtis, Inc. Stable anhydrous topically-active composition and suspending agent therefor
GB9016525D0 (en) * 1990-07-27 1990-09-12 Unilever Plc Cosmetic composition
FR2666962B1 (en) * 1990-09-26 1996-06-14 Oreal ANTIFUNGAL COMPOSITION IN THE FORM OF DRY SPRAY.

Also Published As

Publication number Publication date
ATE227562T1 (en) 2002-11-15
FR2709131B1 (en) 1995-11-10
DE69431700T2 (en) 2004-02-26
EP0639372A1 (en) 1995-02-22
CA2130305A1 (en) 1995-02-19
US5582815A (en) 1996-12-10
FR2709131A1 (en) 1995-02-24
JPH07233091A (en) 1995-09-05
DE69431700D1 (en) 2002-12-19
CA2130305C (en) 2005-12-20

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